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The Longwood Herbal Task Force

(http://www.mcp.edu/herbal/default.htm) and
The Center for Holistic Pediatric Education and Research
(http://www.childrenshospital.org/holistic/)

Identification of Salicin Content of Alcohol Glicoside


White Willow Bark (Salix alba)
Ellen Silver Highfield and Kathi J. Kemper, MD, MPH

Principal Proposed Uses: Analgesic, antipyretic, anti-inflammatory


Other Proposed Uses: Wart remedy

Overview
White willow bark has been used throughout the world as an antipyretic and analgesic.
Since the development of synthetic acetylsalicylic acid in the 1890s, willow bark has fallen into
disuse and has not undergone rigorous scientific evaluation. The concentration of salicin is
actually much lower in willow bark than in other Salix species. The high concentration of tannins
in willow bark (8-20%) usually leads to gastrointestinal toxicity before therapeutic
concentrations of salicylates are achieved. Willow bark does not appear to affect coagulation and
has not been evaluated for use in preventing colorectal cancer, strokes or myocardial infarctions.
Its topical use as an analgesic and wart remover appear safe. Caution suggests avoiding willow
bark in children with influenza or varicella to minimize the risk of Reyes syndrome, and in
patients with asthma, allergies to aspirin, active peptic ulcer disease, diabetes, or hepatic or renal
disorders. There are no data evaluating its safety during pregnancy or lactation.

Historical and Popular Uses


Ancient Egyptians used the bark of the white willow to treat pain and inflammation1.
Hippocrates and Dioscorides recommended willow bark as a remedy for gout and rheumatic
joint diseases, but it fell into disuse in Europe during the Middle Ages. Kuan-Yin, the
bodhisattva of compassion, is often depicted holding a willow branch as a symbol of healing.
Native American healers also relied on willow for its analgesic properties2. The English
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Kathi J. Kemper, MD, MPH Revised July 8, 2014
Longwood Herbal Task Force: http://www.mcp.edu/herbal/default.htm
clergyman Edward Stone rediscovered the therapeutic value of willow bark in 17633. Willow
bark has been used to treat many different kinds of pain, including rheumatic pain, back pain,
toothache, headache, and menstrual cramps. It is also used to relieve sore throat, fever and
headache associated with upper respiratory tract infections and influenza4-6.
Willows active chemical constituent, salicin, was identified in 1829 by the French
pharmacist H. Leroux3. Salicylic acid was prepared in pure form by an Italian chemist in 1838.
Salicylic acid was also extracted from wintergreen, spirea and other plants 3. Salicin and salicylic
acid were widely used by 19th century European physicians to treat rheumatic fever and as an
antipyretic, gout remedy and analgesic, particularly for joint pain4. However, the high doses
used (8-10 grams daily) routinely led to vomiting and gastric irritation, and the search was on for
a less noxious salicylate.
Acetylsalicylic acid was first synthesized by a French chemist in 1853 and was
rediscovered by Felix Hoffman at the Bayer Company in Germany who created acetylsalicylic
acid from the spiric acid (spirin) found in meadowsweet in the 1890s7. Bayer Aspirin quickly
became one of the most popular drugs sold worldwide.
Nowadays, synthetic acetylsalicylic acid is used not only as an analgesic and antipyretic,
but to prevent myocardial infarctions, strokes and colorectal cancer. Some herbalists recommend
willow bark extract as a natural substitute for aspirin to achieve these same benefits. In Germany,
willow bark is often taken along with aspirin to enhance the therapeutic effects while minimizing
side effects8. The European Scientific Cooperative on Phytotherapy (ESCOP) has approved
willow bark extract to treat fever, pain, and mild rheumatic complaints9.

Botany
Medicinal species: Salix alba L (NOTE: There are over 300 Salix species called willow)
Common names: White willow, catkins willow, European willow, salicin willow, withe withy;
Weidenrinde, Fieberweidenrinde, Maiholzrinde (Ger); ecorce de saule (Fr)
Botanical family: Salicaceae
Plant description: Willow trees grow 6-18 meters high with supple branches. The male flowers
are yellow and the female flowers are green. Catkins are cylindrical, approximately 6-7

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Kathi J. Kemper, MD, MPH Revised July 8, 2014
Longwood Herbal Task Force: http://www.mcp.edu/herbal/default.htm
cm long10. The outer surface of the bark can range in color from yellowish-green to
brownish-gray and from a smooth texture to faint longitudinal striations. The inner
surface is smooth and white to pale yellow or cinnamon brown color11.
Where its grown: White willow is native to Europe, Asia and North America. Like birch, it is
very cold hardy. White willow grows in a variety of climates from Maine to the
Amazon12. The bark of young, two- to three-year-old branches is harvested during the
early spring13; it is dried and prepared in liquid, cream, ointment, tablets and capsule
forms. Imports typically come from Bulgaria, Hungary, Romania and the former
Yugoslavia11.

Biochemistry
White Willow Bark: Potentially Active Chemical Constituents11, 14
Glycosides (1.5-11%): salicylates (salicin, salicortin, populin, fragilin, tremulacin)15, 16
Tannins (8-20%)17
Aromatic aldehydes and acids: salidroside, vanillin, syringin, salicylic acid, caffeic and
ferulic acids
Salicyl alcohol (saligenin)
Flavonoids

Salicylates are found in a number of plants including other Salix species, wintergreen
(Gaultheria procumbens), black cohosh root (Cimicifuga racemosa), poplar tree bark (Populus
spp.) and sweet birch tree bark (Betula lenta). Other Salix species (e.g. S. nigra or black willow,
S. daphnoides or violet willow, S. purpurea or purple osier, and S. fragilis or crack willow) are
frequently substituted for white willow in commercial products. Salicylate content appears to be
highest in S. fragilis bark (1-10%), S. purpurea bark (3-9%), S. repens leaves (5-12%), and S.
rosmaninifolia leaves (7-10%) and lowest in white willow bark (1.5-11%)12, 14, 18, 19. The
concentration and availability of salicylates also varies within species according to growing
conditions, processing and preparation15, 20, 21.

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Kathi J. Kemper, MD, MPH Revised July 8, 2014
Longwood Herbal Task Force: http://www.mcp.edu/herbal/default.htm
Salicin and salicortin are the primary salicylates found in white willow bark. They are
metabolized by intestinal flora to saligenin22, absorbed into the blood stream, and metabolized
by the liver to salicylic acid; excretion is primarily renal11, 23. More than 80% of salicin is
absorbed after oral administration24. Because of the time required to metabolize the willows
salicylates, the time to achieve therapeutic effects and the duration of effects are longer than with
synthetic salicylates19, 25.
Salicylic acid is approved by the US Food and Drug Administration (FDA) as a topical
treatment for warts and calluses. It is also included in many non-prescription medications to treat
bunions and corns, and some over the counter acne remedies.
Tannins are phenolic compounds found in many herbs and common foods such as sorrel
and rhubarb. Tannins are astringent and are traditionally used topically to treat wet or oozing
skin conditions such as poison ivy and eczema. Tannins have also been used internally to treat
diarrhea and inflamed mucus membranes. Plants that contain more than 10% tannins have
potential adverse effects including upset stomach and nausea and vomiting acutely, and renal
damage, hepatic necrosis, and increased risk of esophageal and nasal cancer with long term use.
Willow bark contains between 8-20% tannins, a higher concentration than in almost any other
plant. Tannins may interfere with the absorption of alkaloid compounds, salicylic acid, iodine,
zinc, iron and copper. Drug-tannin precipitates may form in alkaline environments, interfering
with proper dosing26.

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Kathi J. Kemper, MD, MPH Revised July 8, 2014
Longwood Herbal Task Force: http://www.mcp.edu/herbal/default.htm
Experimental Studies
White Willow Bark: Potential Clinical Uses
1. Cardiovascular: none
2. Pulmonary: none
3. Renal and electrolyte balance: none
4. Gastrointestinal/hepatic: none
5. Neuro-psychiatric: Analgesic
6. Endocrine: none
7. Hematologic: Anticoagulant and antithrombotic
8. Rheumatologic: Arthritis (See Immune modulation: Anti-inflammatory)
9. Reproductive: none
10. Immune modulation: Anti-inflammatory
11. Antimicrobial: Antifungal
12. Antineoplastic: Prevention of colorectal cancer
13. Antioxidant: none
14. Skin and mucus membranes: none
15. Other/miscellaneous: Antipyretic; wart remedy

With the advent of synthetic aspirin, the use of willow bark fell by the wayside both
clinically and scientifically. Very few studies have addressed the physiologic effects of willow
bark as opposed to aspirin. Modern herbalists have tended to extrapolate the data from studies on
aspirin and apply those findings to willow bark. Studies cited refer to willow bark and/or salicin.

1. Cardiovascular: none
2. Pulmonary: none
3. Renal and electrolyte balance: none
4. Gastrointestinal/hepatic: none
5. Neuro-psychiatric: Analgesic. Salicin does have analgesic properties. However, due to the
low concentration of salicin in willow bark, the amount extracted in typical preparations and
the metabolic transformation required to convert salicin and salicortin to salicylic acid,

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Kathi J. Kemper, MD, MPH Revised July 8, 2014
Longwood Herbal Task Force: http://www.mcp.edu/herbal/default.htm
achieving therapeutic effects would require approximately 35 grams of white willow bark
three times daily. At typical doses, willow bark is not expected to exert significant analgesic
effects19. However, recent unpublished data suggests that willow bark extracts may provide
significant therapeutic benefit even with low salicylate levels.
i. In vitro data: none
ii. Animal data: none
iii. Human data: In a randomized, double-blind placebo-controlled trial of 54 migraine
sufferers, half were given a topical medicament containing salicin (dose unknown) and
half were given a placebo. All were advised that when a headache began, they should lie
down, apply the medicament to their forehead (amount unknown), cover the face with a
photo-occlusive mask and take their regular headache medications. Those treated with
salicin reported significantly more improvement than those assigned to placebo
treatment5.
6. Endocrine: none
7. Hematologic: Anticoagulant and antithrombotic: Some herbalists recommend willow bark as
a natural alternative to aspirin to prevent myocardial infarction and strokes. However,
willows salicylates do not appear to interfere with coagulation.
i. In vitro data: Unlike aspirin, sodium salicylate had no effect on platelet adhesion or
platelet release of ADP27.
ii. Animal data: none
iii. Human data: Unlike aspirin, sodium salicylate did not prolong bleeding time in adults;
nor did it inhibit platelet aggregation27.
8. Rheumatologic: Arthritis (See Immune modulation: Anti-inflammatory)
9. Reproductive: none
10. Immune modulation: Anti-inflammatory
i. In vitro data: Unlike aspirin, salicin did not inhibit PHA-induced lymphocyte
transformation28.
ii. Animal data: none
iii. Human data: Although salicin does have anti-inflammatory properties, the concentration
in willow bark is so low that 25-35 liters of willow bark tea would be required to achieve

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Kathi J. Kemper, MD, MPH Revised July 8, 2014
Longwood Herbal Task Force: http://www.mcp.edu/herbal/default.htm
dosages comparable to 4 grams of aspirin daily. However, a recent unpublished case
series suggests that standardized willow bark extracts may provide significant therapeutic
benefit for patients with rheumatic pain. Randomized controlled trials are underway. See
the report from the International Association for the Study of Pain:
http://www.rzuser.uni-heidelberg.de/%7Ecn6/iasp-sig-rp/willow.html
11. Antimicrobial: Antifungal
i. In vitro data: Aqueous extracts of dried willow bark displayed antifungal activity against
Botrytis cincerea and Penicillium digitatum, but were inactive against Aspergillus
fumigatus, Aspergillus niger, Rhizopus nigricans, Trichophyton mentagrophytes and
Candida albicans29.
ii. Animal data: none
iii. Human data: none
12. Antineoplastic: Prevention of colorectal cancer. No data on willow bark for this use.
13. Antioxidant: none
14. Skin and mucus membranes: none
15. Other/miscellaneous: Antipyretic; wart remedy
a. Antipyretic: no recent scientific evaluation
b. Wart remedy
i. In vitro data: none
ii. Animal data: none
iii. Human data: In central Italy dried willow bark is applied topically to treat warts30; a
modern home remedy is to tape a plain adult aspirin over a wart. There have been no
controlled trials reported on willow barks use for this purpose, but it is likely to be as
effective as other home remedies.

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Kathi J. Kemper, MD, MPH Revised July 8, 2014
Longwood Herbal Task Force: http://www.mcp.edu/herbal/default.htm
Toxicity and Contraindications
All herbal products carry the potential for contamination with other herbal products, pesticides,
herbicides, heavy metals and pharmaceuticals.
Allergic reactions can occur to any natural product in sensitive persons.

Allergic reactions to willow bark have been reported26. Persons known to be allergic to aspirin
should avoid herbal remedies containing willow bark.
Potentially toxic compounds in willow bark: Salicin, salicortin, tannins
Acute toxicity: Toxicity is far less with willow bark than with aspirin due to the low levels of
salicylates in the plant products. High doses can be associated with gastric and renal
irritation, nausea, vomiting, and gastrointestinal bleeding, but side effects are far more
likely from the high tannin levels than the salicylates. There is one case report of a
woman with glucose-6-phosphate dehydrogenase deficiency (G6PD) who developed
massive hemolysis after taking an herbal preparation containing salicin31.
Chronic toxicity: None reported with willow bark, but theoretically possible due to salicylates.
Limitations during other illnesses or in patients with specific organ dysfunction: Patients with
tinnitus should avoid using herbal remedies such as willow bark that contain salicylates.
Although side effects have not been reported, the salicylate content warrants cautious use
by patients with allergies to aspirin, asthma, active peptic ulcer disease, diabetes, gout,
hemophilia and other bleeding disorders, or hepatic or renal disease32.
Interactions with other herbs or pharmaceuticals: None reported. There is a potential for
interaction with salicylate-containing medications and other non-steroidal anti-
inflammatory medications (NSAIDs). There is not expected to be a negative interaction
with anticoagulant medications. Tannins may interfere with absorption of other
medications.
Safety during pregnancy and/or childhood: Due to the potential of developing Reyes syndrome
from salicylates, children with influenza or varicella should avoid willow bark. Safety has
not been established for pregnancy and lactation. Salicylates in breast milk were reported
to cause a rash in one breast-fed baby32.

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Kathi J. Kemper, MD, MPH Revised July 8, 2014
Longwood Herbal Task Force: http://www.mcp.edu/herbal/default.htm
Typical Dosages
Provision of dosage information does NOT constitute a recommendation or endorsement, but
rather indicates the range of doses commonly used in herbal practice.
Doses are given for single herb use and must be adjusted when using herbs in combinations.
Doses may also vary according to the type and severity of the condition treated and individual
patient conditions.

Plants containing salicylates have a very bitter taste, so willow bark tea may be
unpalatable for most patients, particularly for children.
A typical 500 mg dose of aspirin is equivalent to 794 mg of salicin. If extraction was
100% effective, this amount of salicin could be derived from 80-150 grams of dried willow
bark33. The usual dose of willow bark tea is typically 1-3 grams of bark per cup of water. Thus,
the usual herbal products contain minute amounts of salicylates compared with aspirin.

Tea is made by steeping -2 tsp. (1-3 grams) of the dried bark in 1 cup of boiling water for 10-
20 minutes (infusion) or bringing this amount of cold water and dried bark to a boil for 5
minutes (decoction)11, 12. Some herbalists suggest drinking one cup a day to help
prevent myocardial infarction and stroke. To treat fever and pain, 3-5 cups a day are
recommended (containing a total of 60-120 mg of salicin)6. Larger amounts are likely to
lead to gastrointestinal upset due to the high tannin content of the bark.
Tincture or glycerite: tsp. three times daily34
Liquid extract (1:1 in 25% alcohol): 1-3 ml three times daily8, 35
Capsules: Two to three 379 milligram capsules taken every 3-6 hours8
Topically: Infused in vegetable oil and rubbed over painful joints or muscles as needed34
Pediatric dosages: Unknown
Dosages used in herbal combinations: Variable

Ellen Silver Highfield and White Willow Bark Page 9


Kathi J. Kemper, MD, MPH Revised July 8, 2014
Longwood Herbal Task Force: http://www.mcp.edu/herbal/default.htm
See Also:
Willow Bark Clinician Information Summary:
http://www.mcp.edu/herbal/willowbark/willowbark.cis.pdf
Willow Bark Patient Fact Sheet: http://www.mcp.edu/herbal/willowbark/willowbark.ph.pdf
The International Association for the Study of Pain:
http://www.rzuser.uni-heidelberg.de/%7Ecn6/iasp-sig-rp/willow.html

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Kathi J. Kemper, MD, MPH Revised July 8, 2014
Longwood Herbal Task Force: http://www.mcp.edu/herbal/default.htm
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Longwood Herbal Task Force: http://www.mcp.edu/herbal/default.htm
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